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31. 发明授权

US5037828A Piperazine derivatives, uses thereof and pharmaceutical compositions containing them 失效
标题翻译：哌嗪衍生物，其用途和含有它们的药物组合物
公开(公告)号：US5037828A
公开(公告)日：1991-08-06
申请号：US533139
申请日：1990-06-06
申请人： Gisbert Sponer , Harald D. Borbe-Volmer , Jurgen Engel , Bernhard Kutscher , Georg Niebch , Marianne Siebert-Weigel
发明人： Gisbert Sponer , Harald D. Borbe-Volmer , Jurgen Engel , Bernhard Kutscher , Georg Niebch , Marianne Siebert-Weigel
IPC分类号： C07D295/08 , A61K31/495 , A61P9/12 , A61P13/02 , A61P15/00 , C07D295/092
CPC分类号： C07D295/088
摘要： The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a hydroxyl group or a methoxy radical, R.sub.2 is a hydrogen atom or a hyroxyl group and R.sub.3 is a hydrogen atom or a hydroxyl group, with the proviso that R.sub.2 and R.sub.3 are not simultaneously hydrogen atoms when R.sub.1 is a methoxy radical; and the pharmacologically acceptable salts thereof.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.
摘要翻译：本发明提供下列通式的化合物：其中R 1为羟基或甲氧基，R 2为氢原子或羟基，R 3为氢原子或羟基，条件是：当R 1是甲氧基时，R 2和R 3不同时为氢原子; 及其药理学上可接受的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。

32. 发明授权

US4992553A Diamine-platinum (II) complex compounds 失效
标题翻译：二胺 - 铂（II）络合物
公开(公告)号：US4992553A
公开(公告)日：1991-02-12
申请号：US438984
申请日：1989-11-20
申请人： Erwin von Angerer , Norbert Knebel , Helmut Schonenberger , Jurgen Engel
发明人： Erwin von Angerer , Norbert Knebel , Helmut Schonenberger , Jurgen Engel
IPC分类号： C07D209/12 , A61K31/40 , A61K31/555 , A61P35/00 , C07D209/08 , C07D401/12 , C07F15/00
CPC分类号： C07F15/0093
摘要： A compound of the general formula: ##STR1## wherein R.sub.1 is hydrogen, a hydroxy group or a C.sub.2 -C.sub.6 alkanoyloxy group, R.sub.2 is hydrogen or a halogen atom, R.sub.3 is hydrogen or a C.sub.1 -C.sub.6 alkyl group, R.sub.4 is a hydroxy group or a C.sub.2 -C.sub.6 alkanoyloxy group, R.sub.5 is hydrogen or a halogen atom and R.sub.6 is hydrogen or a halogen atom, Alk is a C.sub.2 -C.sub.10 alkylene chain where 4 neighboring CH.sub.2 groups may also be replaced by a 1,4-phenylene ring, A-B is the group HN--CH.sub.2 --CH.sub.2 --NH.sub.2, H.sub.2 N--CH.sub.2 --CH--CH.sub.2 --NH.sub.2 or ##STR2## and R.sub.7 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a phenyl radical and X stands for the equivalent of a physiologically acceptable anion. The compound is useful for the treatment of hormone dependent tumors.
摘要翻译：一种通式如下的化合物，其中R 1是氢，羟基或C 2 -C 6烷酰氧基，R 2是氢或卤原子，R 3是氢或C 1 -C 6烷基，R 4是羟基基团或C 2 -C 6烷酰氧基，R 5是氢或卤素原子，R 6是氢或卤素原子，Alk是C 2 -C 10亚烷基链，其中4个相邻的CH 2基也可以被1,4-亚苯基环取代，AB是基团HN-CH 2 -CH 2 -NH 2，H 2 N-CH 2 -CH-CH 2 -NH 2或R 7，并且R 7是氢原子，C 1 -C 6烷基或苯基，X表示相当于生理上可接受的阴离子。该化合物可用于治疗激素依赖性肿瘤。

33. 发明授权

US4923858A Substituted 3-(n-heterocyclic)-2,6-diaminopyridines and -n-oxides 失效
标题翻译：取代的3-（正 - 杂环）-2,6-二氨基吡啶和 - 氧化物
公开(公告)号：US4923858A
公开(公告)日：1990-05-08
申请号：US352287
申请日：1989-05-16
申请人： Jurgen Engel , Peter Emig , Bernd Nickel , Istvan Szelenyi
发明人： Jurgen Engel , Peter Emig , Bernd Nickel , Istvan Szelenyi
IPC分类号： A61K31/44 , A61K31/535 , A61P25/04 , A61P25/08 , A61P29/00 , C07D401/04 , C07D413/04 , C07D417/04
CPC分类号： C07D401/04 , C07D413/04 , C07D417/04
摘要： Compounds of the general formula: ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen or C.sub.1 -C.sub.6 -alkyl, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, halogen or C.sub.2 -C.sub.6 -alkanoyl, X is oxygen, sulphur or the group --NR.sub.5 and R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkanoyl or benzoyl, m and n in each case may represent the integers 1, 2 or 3 and the phenyl radical A is unsubsituted or is substituted by halogen, nitro, C.sub.1 -C.sub.6 -alkyl, trifluoromethyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, CN, carboxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, phenyl, C.sub.1 -C.sub.6 -alkylphenyl or trifluoromethylphenyl, their pyridine-N-oxides and physiologically acceptable salts thereof, processes for their preparation and medicines containing such compounds as active ingredients.
摘要翻译：通式为：其中基团R 1和R 2相同或不同并且表示氢或C 1 -C 6烷基的通式为：其中R 3和R 4相同或不同，表示氢，C 1 -C 6 - 烷基，羟基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基，卤素或C 2 -C 6 - 烷酰基，X是氧，硫或基团-NR 5和R 5是氢，C 1 -C 6烷基，C 2 -C 6 - 烷酰基或苯甲酰基，m和n各自可以表示整数1,2或3，苯基A未取代或被卤素，硝基，C 1 -C 6 - 烷基，三氟甲基，C 3 -C 7 - 环烷基，羟基，C 1 -C 6 - C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基，氨基，C 1 -C 6 - 烷基氨基，二-C 1 -C 6 - 烷基氨基，C 2 -C 6 - 烷酰基氨基，CN，羧基，C 1 -C 6 - 烷氧基羰基，苯基，C 1 -C 6烷基苯基或三氟甲基苯基，它们的吡啶-N-氧化物及其生理学上可接受的盐，其制备方法和含有活性成分的化合物的药物。

34. 发明授权

US4882452A Process for the preparation of ifosfamide having improved properties 失效
标题翻译：制备具有改善性质的异环磷酰胺的方法
公开(公告)号：US4882452A
公开(公告)日：1989-11-21
申请号：US163586
申请日：1988-03-03
申请人： Jurgen Engel , Siegfried Muller , Werner Laubner
发明人： Jurgen Engel , Siegfried Muller , Werner Laubner
IPC分类号： A61K31/675 , A61P35/00 , C07F9/24 , C07F9/6581 , C07F9/6584
CPC分类号： C07F9/65846
摘要： Ifosfamide having improved properties is obtained by crystallization from a solvent mixture selected from the group consisting of (a) a mixture of diethyl ether and a C.sub.1 -C.sub.3 alkanol or (b) a mixture of diisopropyl ether and a C.sub.1 -C.sub.3 alkanol under specific controlled conditions.
摘要翻译：具有改善性能的异环磷酰胺通过从选自（a）二乙醚和C 1 -C 3链烷醇的混合物的混合溶剂中结晶获得，或（b）二异丙基醚和C 1 -C 3链烷醇的混合物在特定控制下条件。

35. 发明授权

US4730068A Tumor retarding (1,2-diphenyl-ethylenediamine)-platinum(II)-complexes 失效
标题翻译：抗肿瘤剂（1,2-二苯基 - 乙二胺） - 铂（II） - 复合物
公开(公告)号：US4730068A
公开(公告)日：1988-03-08
申请号：US831913
申请日：1986-02-21
申请人： Helmut Schonenberger , Erwin von Angerer , Johann Karl , Margaretha Jennerwein , Jurgen Engel
发明人： Helmut Schonenberger , Erwin von Angerer , Johann Karl , Margaretha Jennerwein , Jurgen Engel
IPC分类号： A61K31/28 , A61P35/00 , C07C45/29 , C07C45/51 , C07C45/56 , C07C47/575 , C07F15/00
CPC分类号： C07F15/0093 , C07C45/298 , C07C45/515 , C07C45/562 , C07C47/575
摘要： There are disclosed antitumor active 1,2-diphenyl-ethylenediamine)-platinum(II)-complex of the general formula ##STR1## wherein R.sub.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl and R.sub.2 is either (1) a halogen atom and the groups R.sub.1, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydrogen C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, or R.sub.2 is (2) a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyloxy group in the 4-position or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and if R.sub.2 is (2) then the groups R.sub.1 and R.sub.3 which are the same or differnt are in the 2 and 6 positions of the phenyl group and are halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, a C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alklanoyloxy group or a halo or C.sub.1 -C.sub.5 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group, with the proviso that R.sub.1 can also be hydrogen and the groups R.sub.4, R.sub.5, and R.sub.6 are the same or different and are hydrogen, halogen, trihalomethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, a C.sub.2 -C.sub.6 -alkanoyloxy group or a halo or C.sub.1 -C.sub.4 -alkanesulfonyloxy substituted C.sub.2 -C.sub.6 -alkanoyloxy group and X is the equivalent of a physiologically compatible anion and process of their production.
摘要翻译：公开了具有通式“IMAGE”I的抗肿瘤活性的1,2-二苯基 - 乙二胺） - 铂（II） - 复合物，其中R 7是氢或C 1 -C 6 - 烷基，R 2是（1）卤素原子，基团R 1，R 3，R 4，R 5和R 6相同或不同，为氢，卤素，三卤甲基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基，或R 2为（2）羟基，C 1 -C 6 - 烷氧基，C 4 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧取代 C 2 -C 6 - 烷酰氧基，如果R 2为（2），则相同或不同的基团R 1和R 3为苯基的2和6位，为卤素，三卤代甲基，C 1 -C 6烷基，羟基， C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 5 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基，条件是R 1也可以是氢，基团R 4，R 5和R 6是相同或不同的氢，卤素，三卤代甲基，C 1 -C 6 - 烷基，羟基，C 1 -C 6 - 烷氧基，C 2 -C 6 - 烷酰氧基或卤素或C 1 -C 4 - 烷磺酰氧基取代的C 2 -C 6 - 烷酰氧基，X等同于生理上相容的阴离子及其生产方法。

36. 发明授权

US4263308A N-Alkoxy-dithienylpiperidines, pharmaceutical compositions thereof and methods of use thereof 失效
标题翻译： N-烷氧基 - 二噻吩基哌啶，其药物组合物及其使用方法
公开(公告)号：US4263308A
公开(公告)日：1981-04-21
申请号：US112100
申请日：1980-01-14
申请人： Jurgen Engel , Axel Kleemann , Ute-Achterrath Tuckermann , Klaus Thiemer
发明人： Jurgen Engel , Axel Kleemann , Ute-Achterrath Tuckermann , Klaus Thiemer
IPC分类号： C07D409/14 , A61K31/4433 , A61K31/445 , C07D333/00 , C07D417/14
CPC分类号： C07D333/00
摘要： There are prepared compounds of the formula ##STR1## where R.sub.1 is hydrogen or hydroxy, R.sub.2 is hydrogen or R.sub.1 and R.sub.2 together represent a second bond between the carbon atoms carrying R.sub.1 and R.sub.2, Alk is a C.sub.2 -C.sub.6 alkylene group, R.sub.3 is a C.sub.3 -C.sub.8 -cycloalkyl group, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.6 -hydroxyalkyl group or a C.sub.2 -C.sub.6 -hydroxyalkoxy-C.sub.1 -C.sub.6 -alkyl group and the groups R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are the same or different and are hydrogen, C.sub.1 -C.sub.6 -alkyl group or halogen atoms, their N-oxides, their quaternary salts and their acid addition salts. There are also described processes for their production. The compounds have a strong bronchospasmolytic activity, antianaphylactic activity and an antihistamine-antiserotonine activity.
摘要翻译：制备式为“IMAGE”的化合物，其中R 1为氢或羟基，R 2为氢或R 1和R 2一起代表携带R1和R2的碳原子之间的第二个键，Alk为C2-C6亚烷基，R3为 C 3 -C 8 - 环烷基，C 1 -C 6烷基，C 1 -C 6羟基烷基或C 2 -C 6羟基烷氧基-C 1 -C 6 - 烷基，R 4，R 5，R 6和R 7基团相同或不同的是氢，C 1 -C 6烷基或卤原子，它们的N-氧化物，它们的季盐和它们的酸加成盐。还描述了其生产方法。该化合物具有强的支气管痉挛分解活性，抗过敏活性和抗组织胺 - 抗血清素活性。

37. 发明授权

US08551977B2 Use of perifosine in combination with antimetabolites for the treatment of benign and malignant oncoses in humans and mammals 有权
标题翻译：使用去糖苷与抗代谢药联合用于治疗人类和哺乳动物的良性和恶性肿瘤
公开(公告)号：US08551977B2
公开(公告)日：2013-10-08
申请号：US12751454
申请日：2010-03-31
申请人： Jurgen Engel , Eckhard Gunther , Herbert Sindermann
发明人： Jurgen Engel , Eckhard Gunther , Herbert Sindermann
IPC分类号： A61K31/70 , A61K31/685
CPC分类号： A61K45/06 , A61K31/685 , A61K2300/00
摘要： The invention relates to the use of alkylphosphocholines in combination with antimetabolite antitumor substances for the treatment of benign and malignant oncoses in humans and animals. It is possible in this connection for the alkylphosphocholines to be employed in a combination according to the invention with one or more antimetabolite antitumor substances. Preferred alkylphosphocholines are described by the Formula II. One such preferred alkylphosphocholine is perifosine.
摘要翻译：本发明涉及将烷基磷酰胆碱与抗代谢物抗肿瘤物质组合用于治疗人和动物中良性和恶性肿瘤的用途。在这方面，可以将本发明的组合中的烷基磷酰胆碱与一种或多种抗代谢物抗肿瘤物质一起使用。优选的烷基磷酰胆碱由式II描述。一种这样优选的烷基磷酸胆碱是丝胶黄素。

38. 发明授权

US07666836B2 Method for the therapeutic management of endometriosis 失效
标题翻译：子宫内膜异位症治疗方法
公开(公告)号：US07666836B2
公开(公告)日：2010-02-23
申请号：US11311363
申请日：2005-12-20
申请人： Hilde Riethmuller-Winzen , Jurgen Engel , Ricardo Felberbaum , Klaus Diedrich , Kupker Wolfgang
发明人： Hilde Riethmuller-Winzen , Jurgen Engel , Ricardo Felberbaum , Klaus Diedrich , Kupker Wolfgang
IPC分类号： A61K38/00 , A61K31/497 , A61K31/519 , A61K31/505
CPC分类号： A61K38/08 , A61K45/06 , A61K2300/00
摘要： The present inventions provides a method for therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction by short term induction treatment with an LH-RH antagonist for 4 to 12 weeks. According to another aspect of the present invention, the short term LH-RH treatment is followed by the combined or separate administration of one or more active agents selected from the group consisting of a contraceptive, preferably an oral contraceptive, a non-steroidal anti-rheumatic agent, an analgetic, an androgen other than a 17-alpha-alkyl substituted testosterone or any combinations thereof. According to a further aspect of the present invention a pharmaceutical composition comprising an LHRH antagonist and one ore more active agents selected from the group consisting of a contraceptive, preferably an oral contraceptive, a non-steroidal anti-rheumatic agent, an analgetic, an androgen other than a 17-alpha-alkyl substituted testosterone or any combinations thereof are provided.
摘要翻译：本发明提供了一种通过LH-RH拮抗剂短期诱导治疗4至12周来治疗子宫内膜组织宫外增生，慢性盆腔疼痛和输卵管阻塞的方法。根据本发明的另一方面，短期LH-RH治疗之后是联合或分开施用一种或多种活性剂，所述活性剂选自避孕药，优选口服避孕药，非类固醇抗生素，风湿药，止痛剂，除17-α-烷基取代的睾酮以外的雄激素或其任何组合。根据本发明的另一方面，包含LHRH拮抗剂和一种或多种选自避孕药，优选口服避孕药，非甾体抗风湿药，止痛剂，雄激素的活性剂的药物组合物提供除17-α-烷基取代的睾酮或其任何组合以外的物质。

39. 发明申请

US20080057124A1 Indolyl-3-glyoxylic acid derivatives having therapeutically valuable properties 审中-公开
标题翻译：具有治疗有价值性质的吲哚基-3-乙醛酸衍生物
公开(公告)号：US20080057124A1
公开(公告)日：2008-03-06
申请号：US11894729
申请日：2007-08-20
申请人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jurgen Engel , Erik Bruyneel , Gunter Kamp , Kirsten Peters
发明人： Bernd Nickel , Gerald Bacher , Thomas Klenner , Thomas Beckers , Peter Emig , Jurgen Engel , Erik Bruyneel , Gunter Kamp , Kirsten Peters
IPC分类号： A61K9/28 , A61K31/404 , A61K31/4427 , A61P35/00 , A61K31/496
CPC分类号： A61K31/496 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4709
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general and to pharmaceutical compositions having antitumor action.
摘要翻译：本发明涉及具有抗肿瘤作用的一般药物组合物和N-取代吲哚-3-乙醛酰胺的用途。

40. 发明申请

US20050124546A1 Oligopeptide lyophilisate, their preparation and use 失效
公开(公告)号：US20050124546A1
公开(公告)日：2005-06-09
申请号：US11039997
申请日：2005-01-24
申请人： Jurgen Engel , Burkhard Wichert , Dieter Sauerbier , Thomas Reissmann
发明人： Jurgen Engel , Burkhard Wichert , Dieter Sauerbier , Thomas Reissmann
IPC分类号： A61K9/00 , A61K9/19 , A61K38/09 , A61K47/26 , A61K38/10 , A61K38/06
CPC分类号： A61K9/0019 , A61K9/19 , A61K38/09 , A61K47/26 , Y10S514/80 , Y10S930/11 , Y10S930/13
摘要： A novel lyophilizate and method of preparation as well as the use of the lyophilizate to treat female infertility and for gonad protection. Cetrorelix is dissolved in acetic acid 30% v/v, the solution is transferred to water and freeze dried.

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